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Flavopiridol Hydrochloride

(CAS No:131740-09-5)
Flavopiridol HCl competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.
CAS No:131740-09-5
Molecular Weight(MW):438.3
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 131740-09-5
Molecular formula(MF) C21H20ClNO5.HCl
Molecular Weight(MW): 438.3
Alias (-)-2-(2-Chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-4H-1-benzopyran-4-one hydrochloride
Solubility
In vitro DMSO 88 mg/mL (200.77 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/mL
Biological Activity
Description Flavopiridol HCl competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.
Targets
CDK1 [1]
(Cell-free assay)		 CDK2 [1]
(Cell-free assay)		 CDK4 [1]
(Cell-free assay)		 CDK6 [1]
(Cell-free assay)		 CDK7 [1]
(Cell-free assay)
40 nM 40 nM 40 nM 40 nM 300 nM
In vitro

Flavopiridol is initially found to inhibit the epidermal growth factor receptor and protein kinase A (IC50 = 21 and 122 μM). Flavopiridol is later shown to inhibit cell proliferation, at more physiologically relevant concentrations (IC50 = 66 nM) when Flavopiridol is tested in the National Cancer Institute Development Therapeutics Program panel of 60 human tumor cell lines. [1] Flavopiridol induces G1 arrest with inhibition of CDK2 and CDK4 in human breast carcinoma cells in a time and concentration dependent manner. [2] Short time treatment of Flavopiridol (~12 hours) induce apoptosis in hematopoietic cell lines including SUDHL4, SUDHL6 (B-cell lines), Jurkat and MOLT4 (T-cell lines ), and HL60 (myeloid). [3] In the clonogenic assay, Flavopiridol functions as a highly potent cytotoxic compound with a mean IC70 with 8 ng/mL in 23 human tumor models. [4] A recent study shows Flavopiridol treatment induces a substantial AKT-Ser473 phosphorylation in human glioblastoma T98G cell line. [5]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ID8 cells Proliferation assay Antiproliferative activity against ID8 cells, IC50=7 nM 17123821
Sf9 cells Function assay Inhibition of recombinant cyclin A/CDK2 expressed in Sf9 cells, IC50=12 nM 17904366
LNCaP human prostate carcinoma cell Proliferation assay Inhibition of LNCaP human prostate carcinoma cell proliferation 12190313
HCT116/VP35 human colon carcinoma cell Proliferation assay Inhibition of HCT116/VP35 human colon carcinoma cell proliferation, IC50=17 nM 12190313
HCT116 human colon carcinoma cell Proliferation assay Inhibition of HCT116 human colon carcinoma cell proliferation, IC50=18 nM 12190313
HCT116/VM46 human colon carcinoma cell Proliferation assay Inhibition of HCT116/VM46 human colon carcinoma cell proliferation, IC50=21 nM 12190313
human A2780 cells Cytotoxic assay 24 h Cytotoxicity against human A2780 cells after 24 hrs by MTT assay, GI50=23 nM 23301767
MCF7 cells Proliferation assay Antiproliferative activity against MCF7 cells, IC50=26 nM 17123821
human MRC5 cells Cytotoxic assay 72 h Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay, GI50=28 nM 23301767
human A2780 cells Cytotoxic assay 72 h Cytotoxicity against human A2780 cells after 72 hrs by MTT assay, GI50=29 nM 23301767
human A2780 cells Cytotoxic assay 48 h Cytotoxicity against human A2780 cells after 48 hrs by MTT assay, GI50=31 nM 23301767
A2780/DDP-R human ovarian carcinoma cell Proliferation assay Inhibition of A2780/DDP-R human ovarian carcinoma cell proliferation, IC50=38 nM 12190313
human MRC5 cells Cytotoxic assay 48 h Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay, GI50=39 nM 23301767
ABAE human fibroblast cell Proliferation assay Inhibition of ABAE human fibroblast cell proliferation, IC50=45 nM 12190313
HL60 human leukemia cell Proliferation assay Inhibition of HL60 human leukemia cell proliferation, IC50=46 nM 12190313
human MRC5 cells Cytotoxic assay 24 h Cytotoxicity against human MRC5 cells after 24 hrs by MTT assay, GI50=49 nM 23301767
Hs 27 human fibroblast cell Proliferation assay Inhibition of Hs 27 human fibroblast cell proliferation, IC50=51 nM 12190313
CCRF-CEM human leukemia cell Proliferation assay Inhibition of CCRF-CEM human leukemia cell proliferation, IC50=52 nM 12190313
OVCAR-3 human ovarian carcinoma cell Proliferation assay Inhibition of OVCAR-3 human ovarian carcinoma cell proliferation, IC50=54 nM 12190313
A2780/DDP-S human ovarian carcinoma cell Proliferation assay Inhibition of A2780/DDP-S human ovarian carcinoma cell proliferation, IC50=56 nM 12190313
human HMEC1 cells Cytotoxic assay 24 h Cytotoxicity against human HMEC1 cells after 24 hrs by MTT assay, GI50=61 nM 23301767
human HMEC1 cells Cytotoxic assay 48 h Cytotoxicity against human HMEC1 cells after 48 hrs by MTT assay, GI50=62 nM 23301767
A2780/TAX-S human ovarian carcinoma cell Proliferation assay Inhibition of A2780/TAX-S human ovarian carcinoma cell proliferation, IC50=65 nM 12190313
LS174T human colon carcinoma cell Proliferation assay Inhibition of LS174T human colon carcinoma cell proliferation, IC50=65 nM 12190313
MCF-7 human breast carcinoma cell Proliferation assay Inhibition of MCF-7 human breast carcinoma cell proliferation, IC50=66 nM 12190313
human HMEC1 cells Cytotoxic assay 72 h Cytotoxicity against human HMEC1 cells after 72 hrs by MTT assay, GI50=66 nM 23301767
PC3 human prostate carcinoma cell Proliferation assay Inhibition of PC3 human prostate carcinoma cell proliferation, IC50=66 nM 12190313
human A2780 cell line Proliferation assay 72 h Antiproliferative effect against human A2780 cell line was determined in a whole cell 72 hr cytotoxicity assay, IC50=71 nM 15027863
human ovarian (A2780) cancer cell Cytotoxic assay Cytotoxic effect on human ovarian (A2780) cancer cell line, IC50=71 nM 15125971
MLF mouse lung fibroblast cell Proliferation assay Inhibition of MLF mouse lung fibroblast cell proliferation, IC50=72 nM 12190313
human NCI60 cells Proliferation assay 72 h Antiproliferative activity against human NCI60 cells after 72 hrs by sulforhodamine B assay, GI50=74.7 nM 21080703
LX-1 human lung carcinoma Proliferation assay Inhibition of LX-1 human lung carcinoma proliferation, IC50=75 nM 12190313
A431 human squamous cell Proliferation assay Inhibition of A431 human squamous cell carcinoma cell proliferation, IC50=75 nM 12190313
SKBR-3 human breast carcinoma cell Proliferation assay Inhibition of SKBR-3 human breast carcinoma cell proliferation, IC50=77 nM 12190313
A2780/TAX-R human ovarian carcinoma cell Proliferation assay Inhibition of A2780/TAX-R human ovarian carcinoma cell proliferation, IC50=78 nM 12190313
M109 mouse lung carcinoma cell Proliferation assay Inhibition of M109 mouse lung carcinoma cell proliferation, IC50=80 nM 12190313
CACO-2 human colon carcinoma cell Proliferation assay Inhibition of CACO-2 human colon carcinoma cell proliferation, IC50=86 nM 12190313
A549 human lung carcinoma cell Proliferation assay Inhibition of A549 human lung carcinoma cell proliferation, IC50=96 nM 12190313
MIP human colon carcinoma cell Function assay Inhibition of MIP human colon carcinoma cell line, IC50=0.12 μM 12190313
K562 human leukemia cell Proliferation assay Inhibition of K562 human leukemia cell proliferation, IC50=0.13 μM 12190313
MCF-7 tumor cell Proliferation assay Inhibition of MCF-7 tumor cell proliferation 10843211
human NCI60 cells Proliferation assay 72 h Antiproliferative activity against human NCI60 cells assessed as lethal effect after 72 hrs by sulforhodamine B assay, LC50=0.904 μM 21080703
PC3 cell Function assay Inhibition of PC3 cell clonogenic assay, IC50=10 μM 11063609
HCT116 cell Function assay Inhibition of HCT116 cell clonogenic assay, IC50=13 μM 11063609
A2780 cell Function assay Inhibition of A2780 cell clonogenic assay， IC50=15 μM 11063609
Mia PaCa-2 cell Function assay Inhibition of Mia PaCa-2 cell clonogenic assay, IC50=36 μM 11063609
human A2780 cells Function assay Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells 18469809
human A2780 cells Function assay 24 h Inhibition of cdk-mediated Rb phosphorylation at thr821 in human A2780 cells after 24 hrs 18469809

... Click to View More Cell Line Experimental Data
In vivo At the maximal tolerated dose of 10 mg/kg/day administered p.o. on days 1-4 and 7-11, Flavopiridol effects tumor regression in PRXF1337 and tumor stasis lasting for 4 weeks in PRXF1369. [4] After treatment with 7.5 mg/kg Flavopiridol bolus intravenous (IV) or intraperitoneal on each of 5 consecutive days, 11 out of 12 advanced stage subcutaneous (s.c.) human HL-60 xenografts undergo complete regressions, and animals remain disease-free several months after one course of Flavopiridol treatment. SUDHL-4 s.c. lymphomas treated with flavopiridol at 7.5 mg/kg bolus IV for 5 days undergo either major (two out of eight mice) or complete (four out of eight mice) regression, with two animals remaining disease-free for more than 60 days. The overall growth delay is 73.2%. Daily IV or IP administration of flavopiridol results in peak plasma levels of about 7 µM, followed by a progressive decline to approximately 100 nM in 8 hours.[6]
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